Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (1), p.78-82
2010
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (1), p.78-82
- Ort / Verlag
- England
- Erscheinungsjahr
- 2010
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Syntheses, biological evaluation, and structure-activity relationships for a series of novel 5-styryl and 5-phenethyl analogs of dimebolin are disclosed. The novel derivatives and dimebolin share a broad spectrum of activities against therapeutically relevant targets. Among all synthesized derivatives, 2,8-dimethyl-5-[(Z)-2-phenylvinyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole and its 5-phenethyl analog are the most potent blockers of 5-HT(7), 5-HT(6), 5-HT(2C), Adrenergic alpha(2) and H(1) receptors. The general affinity rank order towards the studied receptors was Z-3(2)>4(2)4(3)>>dimebolin, all of them having highest affinities to 5-HT(7) receptors.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2009.11.037Titel-ID: cdi_proquest_miscellaneous_733950566
- Format
- –
- Schlagworte
- Adrenergic alpha-2 Receptor Antagonists, Adrenergic alpha-Antagonists - chemical synthesis, Adrenergic alpha-Antagonists - chemistry, Adrenergic alpha-Antagonists - pharmacology, Cell Line, Histamine H1 Antagonists - chemical synthesis, Histamine H1 Antagonists - chemistry, Histamine H1 Antagonists - pharmacology, Humans, Indoles - chemical synthesis, Indoles - chemistry, Indoles - pharmacology, Receptor, Serotonin, 5-HT2C - metabolism, Receptors, Adrenergic, alpha-2 - metabolism, Receptors, Histamine H1 - chemistry, Receptors, Histamine H1 - metabolism, Receptors, Serotonin - chemistry, Receptors, Serotonin - metabolism, Serotonin 5-HT2 Receptor Antagonists, Structure-Activity Relationship